伏立康唑微乳化水凝胶的配方及体外经皮渗透和皮肤蓄积的研究

M. Prajapati, S. Shende, V. Jain, A. Gupta, Manoj Kumar Goyal
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摘要

本研究的目的是制备伏立康唑微乳化水凝胶并对其进行评价。采用水滴定法制备伏立康唑微乳化剂。将伏立康唑微乳化后掺入水凝胶,用蒸馏水制备不同聚合物的空白凝胶。最后,将0.5%卡波波尔w/v和0.5%芦荟粉分散于100ml水中,机械搅拌,制备卡波波尔凝胶。此外,为了保存配方,混合了0.8%的对羟基苯甲酸甲酯。将伏立康唑纯品溶于油酸、蓖麻油、椰子油、橄榄油、籽粒矿物油和大豆油中,选择油相。根据伏立康唑在其中的溶解度较高,选择了油酸。通过清晰的目视观察,选择表面活性剂和助表面活性剂的组合。Span - 40:丙二醇以1:1和2:1的比例进一步制备微乳液。从研究中选择F-8、F-9、F-10、F-14和F-15进行进一步研究。虽然F-16、F-17、F-18、F-19和F-20的配方也很稳定,但由于表面活性剂浓度高,会引起皮肤刺激、皮肤灼烧和/或其他并发症而被拒绝。通过液滴大小、Zeta电位、聚分散指数(PDI)和药物含量(%)等参数对优选的伏立康唑微乳配方进行表征。
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Formulation and In vitro Percutaneous Permeation and Skin accumulation of Voriconazole Microemulsified Hydrogel
The aim of the present study was to prepare and evaluate voriconazole microemulsified hydrogel. The voriconazole microemulsified is prepared by Water Titration Method. In which voriconazole microemulsified incorporated with hydrogel, Blank gels of different polymers were prepared by distilled water. Finally, the carbopol gel was prepared by dispersing 0.5% carbopol w/v and 0.5% aloe vera powder in 100 ml of water with stirring on mechanical stir. Additionally, for preservation of formulations 0.8% methyl paraben was mixed. Oil phase was selected by dissolving the voriconazole pure in different oils, oleic acid, castor oil, coconut oil, olive oil, cooten seed mineral oil and soya oil. Oleic acid was selected on the basis of higher solubility of voriconazole in it. Combination of surfactant and co-surfactant was selected on clear visual observation. Span - 40: propylene glycol in ratio 1:1 and 2:1 selected for further preparation of microemulsion. From the study F-8, F-9, F-10, F-14 and F-15 were selected for further studies. Though F-16, F-17, F-18, F-19 and F-20 formulations are also stable, but rejected due to high concentration of surfactant can cause skin irritation, skin burning and/or other complications. Characterization of selected voriconazole microemulsion formulations were evaluated under various parameters like Droplet size, Zeta potential, Poly Dispersity Index (PDI) and (%) Drug content all results showed.
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